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Submit ReviewDecanoyl-RVKR-CMK
Description: Subtilisin/Kex2p-like proprotein convertase inhibitor
Purity: ≥95% (HPLC)
Biological Activity for Decanoyl-RVKR-CMK
Decanoyl-RVKR-CMK is a subtilisin/Kex2p-like proprotein convertase inhibitor; blocks activity of all seven convertases (PC1, PC2, PC4, PACE4, PC5, PC7 and furin). Abolishes proET-1 processing in endothelial cells; inhibits regulated secretion of the neuronal polypeptide VGF in PC12 cells. Inhibits cleavage of glycoprotein B of human cytomegalovirus. Also inhibits cleavage of SARS-CoV-2 spike protein by furin and blocks viral cell entry (IC50 = 57 nM in plaque reduction assay).
Technical Data for Decanoyl-RVKR-CMK
| M. Wt | 744.42 |
| Formula | C34H66ClN11O5 |
| Sequence |
RVKR (Modifications: Arg-1 = Decanoyl-Arg, Arg-4 = chlororomethylketone) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 150113-99-8 |
| PubChem ID | 9962075 |
| InChI Key | NHBJTTGFHCHQHS-VZTVMPNDSA-N |
| Smiles | [H]N([C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)CCl)C(=O)CCCCCCCCC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Decanoyl-RVKR-CMK
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for Decanoyl-RVKR-CMK
References for Decanoyl-RVKR-CMK
References are publications that support the biological activity of the product.
Garcia et al (2005) A prohormone convertase cleavage site within a predicted alpha-helix mediates sorting of the neuronal and endocrine polypeptide VGF into the regulated secretory pathway. J.Biol.Chem. 280 41595 PMID: 16221685
Tian and Jianhua (2010) Comparative study of the binding pocket of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors. Int.J.Biol.Sci. 6 89 PMID: 20151049
Denault et al (1995) Inhibition of convertase-related processing of proendothelin-1. J.Cardiovasc.Pharmacol. 26 S47 PMID: 8587448
Cheng et al (2020) Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects. Cell Rep. 33 108254 PMID: 33007239
Vey et al (1995) Proteolytic processing of human cytomegalovirus glycoprotein B (gpUL55) is mediatedby the human endoprotease furin. Virology 206 746 PMID: 7726996
If you know of a relevant reference for Decanoyl-RVKR-CMK, please let us know.
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Keywords: Decanoyl-RVKR-CMK, Decanoyl-RVKR-CMK supplier, proprotein, convertases, inhibitors, inhibits, supplier, proteolytic, cleavage, calcium, dependent, serine, endopeptidases, furin, PC1, PC2, PC4, PACE4, PC5, PC7, secretory, pathway, MERS, SARS, Other, Proteases, Furin, 3501, Tocris Bioscience
13 Citations for Decanoyl-RVKR-CMK
Citations are publications that use Tocris products. Selected citations for Decanoyl-RVKR-CMK include:
Wei et al (2023) A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry. Cell 186 850-863.e16 PMID: 36803605
Jurga et al (2023) High-throughput measurement of the content and properties of nano-sized bioparticles with single-particle profiler. Nat Biotechnol PMID: 37308687
Cheng et al (2020) Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects. Cell Rep. 33 108254 PMID: 33007239
Hoffman et al (2020) A Multibasic Cleavage Site in the Spike Protein of SARS-CoV-2 Is Essential for Infection of Human Lung Cells. Mol Cell 78 779 PMID: 32362314
Wang et al (2019) Biowire Model of Interstitial and Focal Cardiac Fibrosis. ACS Cent Sci 5 1146 PMID: 31403068
Robert F et al (2021) SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation. Elife 10 PMID: 33890572
Dong et al (2021) Host and viral determinants for efficient SARS-CoV-2 infection of the human lung. Nat Commun 12 134 PMID: 33420022
Michael et al (2017) Cutting Edge: ERK1 Mediates the Autocrine Positive Feedback Loop of TGF-β and Furin in Glioma-Initiating Cells. J Immunol 198 4569-4574 PMID: 28484053
Robert W et al (2022) A Newly Engineered A549 Cell Line Expressing ACE2 and TMPRSS2 Is Highly Permissive to SARS-CoV-2, Including the Delta and Omicron Variants. Viruses 14 PMID: 35891350
Henrik et al (2020) The half-life of the bone-derived hormone osteocalcin is regulated through O-glycosylation in mice, but not in humans. Elife 9 PMID: 33284103
Matsuyama et al (2018) Middle East Respiratory Syndrome Coronavirus Spike Protein Is Not Activated Directly by Cellular Furin during Viral Entry into Target Cells. J Virol 92 PMID: 30021905
Millet & Whittaker (2014) Host cell entry of Middle East respiratory syndrome coronavirus after two-step, furin-mediated activation of the spike protein. Proc Natl Acad Sci U S A 111 15214 PMID: 25288733
Edin (2014) The role of interleukin-13 in the removal of hyper-radiosensitivity by priming irradiation. Am J Physiol Gastrointest Liver Physiol 55 1066 PMID: 24966400
Do you know of a great paper that uses Decanoyl-RVKR-CMK from Tocris? Please let us know.
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